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other·nutrition, clinical nutrition, preclinical research, research methods·PMC10610233

Flavonoids in the Spotlight: Bridging the Gap between Physicochemical Properties and Formulation Strategies

Pharmaceuticals · 5 authors, 1 centre

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TL;DR

Most flavonoids were classified as poorly soluble compounds with limited absorption windows in the upper small intestine.

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Most flavonoids were classified as poorly soluble with relatively high or low permeability (Class IIa/IIb) or low permeability (Class IV). The Bagley plot analysis indicated an absorption window in the upper small intestine with limited absorption time. A key gap identified was the paucity of experimental pKa, permeability, solubility, and recommended maximum daily dose data for many flavonoids. The authors concluded that enabling formulations are needed for Class IIa/IIb and IV flavonoids to improve bioavailability reproducibility.

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other

SPECIALTY

nutrition

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100% · A

ORIGINAL PAPER

PMC10610233

Flavonoids in the Spotlight: Bridging the Gap between Physicochemical Properties and Formulation Strategies

Pharmaceuticals

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ABSTRACT

Abstract Flavonoids are hydroxylated polyphenols that are widely distributed in plants with diverse health benefits. Despite their popularity, the bioavailability of flavonoids is often overlooked, impacting their efficacy and the comparison of products. The study discusses the bioavailability-related physicochemical properties of flavonoids, with a focus on the poorly soluble compounds commonly found in dietary supplements and herbal products. This review sums up the values of p K a , log P , solubility, permeability, and melting temperature of flavonoids. Experimental and calculated data were compiled for various flavonoid subclasses, revealing variations in their physicochemical properties. The investigation highlights the challenges posed by poorly soluble flavonoids and underscores the need for enabling formulation approaches to enhance their bioavailability and therapeutic potential. Compared to aglycones, flavonoid glycosides (with sugar moieties) tend to be more hydrophilic. Most of the reviewed aglycones and glycosides exhibit relatively low log P and high melting points, making them “brick dust” candidates. To improve solubility and absorption, strategies like size reduction, the potential use of solid dispersions and carriers, as well as lipid-based formulations have been discussed. Keywords: flavonoids, physiochemical properties, solubility, p K a , log P , permeability, solubility parameters, brick dust, grease balls, developability classification system

CITATION EXPORT

Marta Berga, Konstantins Logviss, Liga Lauberte et al.. Flavonoids in the Spotlight: Bridging the Gap between Physicochemical Properties and Formulation Strategies. Pharmaceuticals. (2023). https://doi.org/10.3390/ph16101407

AUTHORS

5 · 1 CENTRES

Marta Berga, Konstantins Logviss, Liga Lauberte, Artūrs Paulausks, Valentyn Mohylyuk

1Laboratory of Finished Dosage Forms, Faculty of Pharmacy, Riga Stradiņš University, LV-1007 Riga, Latvia